Showing papers by "Central Drug Research Institute published in 1970"
TL;DR: A systematic study of small free-living amoebae has been made under standardized and reproducible cultural conditions, and their pathogenicity has been tested in mice, and metronidazole and other anti-amoebic drugs are ineffective against N. aerobia and H. culbertsoni in vitro and in meningo-encephalitis in mice.
Abstract: A systematic study of small free-living amoebae has been made under standardized and reproducible cultural conditions, and their pathogenicity has been tested in mice. Naegleria aerobia, Hartmannella culbertsoni and H. rhysodes are pathogenic; H. castellanii, H. astronyxis, H. palestinensis, H. glebae, H. exundans, H. vermiformis, Schizopyrenus russelli, Didascalus thorntoni and Tetramitus rostratus are non-pathogenic. Strains of H. culbertsoni and H. rhysodes are present in Indian soils. A classification of the order Amocbida Kent into families Schizopyrenidae Singh, Hartmannellidae Volkonsky, 1931 emend. Singh, 1952, and Endamoebidae (Calkins), based on nuclear division, is proposed, and the relation of this classification to previously defined families and genera of amoebae and its bearing on phylogeny are discussed. Metronidazole and other anti-amoebic drugs are ineffective against N. aerobia and H. culbertsoni in vitro and in meningo-encephalitis in mice.
108 citations
53 citations
TL;DR: Subtoxic doses of alpha-chlorohydrin were fed to 5 adult male rhesus monkeys in an attempt to produce functional sterility, and the only significant changes were increased zinc-65 uptake and oxygen consumption by vasal spermatozoa.
34 citations
TL;DR: The results indicate the functioning of the glycolytic pathway in this worm which resembles Schistosoma mansoni, a lactic acid producer, in the differential activities of the terminal enzymes of the pathway.
24 citations
TL;DR: Glycogen reserves of whole worms and their body wall, intestines, ovarian and testicular tubules of Ascaridia galli, were assayed and on dry-weight basis found to be 14-20 %, except in the testicular tissue which contained only 7 % glycogen.
Abstract: Glycogen reserves of whole worms and their body wall, intestines, ovarian and testicular tubules of the avian intestinal nematode, Ascaridia galli, were assayed and on dry-weight basis found to be 14–20 %, except in the testicular tissue which contained only 7 % glycogen.Segments of whole male worms or testicular tubules were found to produce more lactic acid than segments of whole female worms or ovarian tubules. The body wall and intestine of the worms had also appreciable glycolytic activity. Whereas in the segments of whole worms, male and female alike, glycolysis was more active under anaerobic conditions, no differences in glycolytic rates were seen between aerobiosis and anaerobiosis when isolated tissues were used. Exogenously added glucose did not stimulate glycolysis either aerobically or anaerobically to any extent greater than observed in the absence of glucose.Homogenates of whole worms or their different anatomical parts were assayed for enzymic activities associated with the Embden-Meyerhof pathway of glucose assimilation. The crude extracts prior to differential centrifugation, were found to contain glycogen phosphorylase, aldokinases, pyruvate kinase, phosphatases acting on glucose 6-phosphate and hexose diphosphate and 6-phospho-gluconate dehydrogenase. The 105000 g particulate-free supernate was found to have significant activities of the following enzymes: fructokinase, phosphoglucomutase, phosphoglucoseisomerase, phosphofructokinase, aldolase, glyceraldehyde 3-phosphate dehydrogenase, lactic dehydrogenase and glucose-6-phosphate dehydrogenase. This fraction was devoid of NADH or NADPH oxidase activities in the absence of added substrates.Although there was some indication of a negative correlation between low glycogen reserves and high glycolytic activity in the testicular tubules, in general, there was no relationship between glycogen reserve and glycolytic activity on the one hand or between the rate of glycolysis and the specific activities of some of the key glycolytic enzymes in either whole worm or in tissues other than the testicular tubules.The 105000 g supernate was fractionated with ammonium sulphate. The fraction precipitating between 25 and 80 % saturation of the salt was recovered, dialysed and chromatographed on DEAE cellulose column. By a step-wise elution schedule using increasing molarity of NaCl in tris-HCl buffer, pH 7·4, three main protein fractions were obtained representing respectively enolase, aldolase and glucose-6-phosphate dehydrogenase.The recovery of enzyme activity after chromatography on DEAE cellulose was higher than the amount applied to the column suggesting that during the fractionation some naturally occurring inhibitors were removed. About 10- to 20-fold purification of the enzymes was achieved by anion-exchange chromatography.Some properties of the purified enzymes were studied with respect to the affects of enzyme and substrate concentrations, temperature of preincubation and action of divalent cations, some anions, metal chelating agents and SH reagents. The Km values of enolase, aldolase and glucose-6-phosphate dehydrogenase of A. galli were 5·9 × 10−4M, 4·5 × 10−3M and 2·4 × 10−3M respectively. Glucose-6-phosphate dehydrogenase was found to be very sensitive to both heat and cold losing activity rapidly even at 43 °C or by freezing and thawing.The SH groups of aldolase were readily blocked by pCMB and presumably by o–phenanthroline. No requirement of any divalent cations was shown by this enzyme which was, however, inhibited by borate ions.Enolase of A. galli showed a requirement of Mg2+ for full activation. Phosphate, fluoride, EDTA, o–phenanthroline, αα-bipyridyl inhibited the enzyme. Veronal was found to inactivate the enzyme.Glucose-6-phosphate dehydrogenase of A. galli was also found to be sensitive to SH reagents and metal chelating agents. The enzyme was activated by Co2+, Mn2+ and Mg2+.The evidence presented indicates that segments of whole worms of A. galli or its anatomical parts are equipped with the enzymatic machinery required to mediate anaerobic breakdown of glucose and to derive energy by this mechanism.The authors are grateful to Dr R. K. Kaushik for help in identifying the worms, to Mr P. A. George for help in the statistical analysis of the data and to Messrs A. C. Kol and S. K. Bose for skilful technical assistance.
22 citations
TL;DR: Three proaporphine bases provisionally designated crotsparine (I), m.p. 125-127°, and two dihydropro-pro-parphines (Crotsparinine (II) and N -methyl-crotsparines (V) have been isolated from Croton sparsiflorus Morong and their structures and stereochemistry assigned as discussed by the authors.
22 citations
TL;DR: The 2-phenyl-3-p-(β-pyrrolidinoethoxy)-phenyl (2:1,b) naphthofuran compound causes 100% prevention of conception in rats, mice, and rhesus monkeys at a single oral dose and has a favorable therapeutic index.
21 citations
TL;DR: Solid incrustations appearing on Lippes loops which had been used from 15-40 months and removed for intractable vaginal bleeding were analysed and mainly protein, calcium, magnesium, carbonate, and a trace of iron and phosphate were found.
20 citations
TL;DR: Ein Biscoclaurin Alkaloid, Pendulin (C37H40N2O6), mp 192–194°, [α]D + 265°, wurde aus Blättern und Stamm von Cocculus pendulus Diels isoliert und seine Struktur (I) inklusive der sterischen Anordnung an beiden Asymetriezentren aufgeklärt.
Abstract: Ein Biscoclaurin Alkaloid, Pendulin (C37H40N2O6), mp 192–194°, [α]D + 265°, wurde aus Blattern und Stamm vonCocculus pendulus Diels isoliert und seine Struktur (I) inklusive der sterischen Anordnung an beiden Asymetriezentren aufgeklart.
17 citations
TL;DR: In the guinea pig, phenylethyl configuration with OH groups at para and meta positions of the phenyl ring does not seem to be an essential criterion for inducing Gnawing as suggested for the rat (Ernst, 1965).
Abstract: 20 compounds acting on the central nervous system and the autonomic nervous system were tested in guinea pigs for their ability to induce gnawing. Only methylphenidate induced vigorous gnawing similar to that produced by apomorphine and amphetamine. Methylphenidate differs in its mode of action from both apomorphine and amphetamine. In the guinea pig, phenylethyl configuration with OH groups at para and meta positions of the phenyl ring does not seem to be an essential criterion for inducing gnawing as suggested for the rat (Ernst, 1965). Catecholamines do not appear to play any significant role in the mediation of methylphenidate gnawing, or even in the gnawing response itself in guinea pigs, since increase in the level of dopamine and other catecholamines does not induce gnawing.
16 citations
TL;DR: Mit N-Bromsuccinimid können Nukleoside in Dimethylformamid mit guter Ausbeute zu den in 5-Stellung bromierten Derivaten umgewandelt werden.
Abstract: Mit N-Bromsuccinimid konnen Nukleoside in Dimethylformamid mit guter Ausbeute zu den in 5-Stellung bromierten Derivaten umgewandelt werden.
TL;DR: Aus den Blättern vonAlstonia scholaris R. Br.
Abstract: Aus den Blattern vonAlstonia scholaris R. Br. sind Pikrinine (Ia), Akuammidine und ein neues, bisher in Pflanzen nicht gefundenes Alkaloid, Pikralinal (Ib) isoliert worden. Pikralinal ist eine SchlUsselsubstanz fUr die Biosynthese vieler Alkaloide des Pikralimatypus.
TL;DR: Ein neuesbisbenzylisochinolines Alkaloid vom Typ des Trilobins wird Cocsulin genannt, (C35H34N2O5), Schmp.
Abstract: Ein neuesbisbenzylisochinolines Alkaloid vom Typ des Trilobins wird Cocsulin genannt, (C35H34N2O5), Schmp. 272–274°, [α]d+280°, und ist aus Blattern und Stamm vonCocculus pendulus Diels isoliert und als Struktur V angegeben worden.
TL;DR: Only the development of solid phase combinatorial synthetic approaches of small nitrogen heterocycles since 1999 will be reviewed here.
Abstract: Recognizing the potential of combinatorial chemistry to accelerate drug discovery and development, most pharmaceutical and related industries are seriously looking toward combinatorial synthesis of compounds in order to facilitate the identification of 'lead' molecules. In particular, solid phase synthesis is the core technology for combinatorial chemistry and is widely used for generating libraries of structurally related compounds. Since many drugs contain the nitrogen heterocyclic component and since heterocycles possess a high order of structural diversity, a precise overview of recent progress in the combinatorial synthesis of nitrogen heterocycles using solid phase methodology would be useful. Since the progress in solid phase synthesis of organic molecules has been reviewed regularly from 1992 to 1998, only the development of solid phase combinatorial synthetic approaches of small nitrogen heterocycles since 1999 will be reviewed here. This review describes the solid phase synthesis of azepanes, benzodiazepines, benzimidazoles, benzothiazepines, cinnolines, indolizines, beta lactams, oxazepins, oxazoles including benzisooxazoles, hydantoins, piperidines, pyrimidines, pyrazolones, quinolones, trizolopyridazines and thiazoles.
TL;DR: Die Struktur (III) des Mahanimbinins, eines Verwandten aus den Blättern vonMurraya koenigii Spreng, ist spektroskopisch und durch Synthese aufgeklärt worden.
Abstract: Die Struktur (III) des Mahanimbinins, eines Verwandten des Mahanimbins aus den Blattern vonMurraya koenigii Spreng., ist spektroskopisch und durch Synthese aufgeklart worden.
TL;DR: Air-dried blood smears and erythrocyte suspension from patients infected with Plasmodium falciparum permit easy detection of plasmodia with fluorescence microscopy together with a clear cytochemical colour differentiation of nuclear DNA and cytoplasmic RNA.
Abstract: Air-dried blood smears and erythrocyte suspension from patients infected with Plasmodium falciparum, stained under optimal conditions with acridine orange, permit easy detection of plasmodia with fluorescence microscopy together with a clear cytochemical colour differentiation of nuclear DNA (green or green-yellow) and cytoplasmic RNA (orange-red fluorescence). Judging from fluorescence characteristics of nuclei (DNase sensitive and RNase resistant green or green-yellow), the plasmodial DNA appears to be double-stranded.
TL;DR: The minimum effective dose was found to be 5 μg/15 days which caused 100% reduction in fertility without disturbing spermatogenesis or libido, however, when the treatment period was extended for 30 days varying degrees of sperMatogenic interruption and loss of libido were recorded.
TL;DR: Possibility of α‐adrenoceptors in the neurones integrating FR is suggested, and effects of some α‐ and β‐ adrenoceptor stimulants and antagonists were investigated on flexor reflex (FR) in chloralosed cats.
Abstract: 1. Effects of some alpha- and beta-adrenoceptor stimulants and antagonists were investigated on flexor reflex (FR) in chloralosed cats.2. Noradrenaline (NA) produced facilitation of FR which was dose-dependent and reproducible and was blocked by alpha-adrenoceptor blocking agents.3. Strychnine also produced facilitation of FR but the response was unaffected by alpha-adrenoceptor blocking agents.4. Metaraminol and alpha-methyl-noradrenaline had little effect on FR but blocked the NA response.5. beta-adrenoceptor stimulants and antagonists had neither any effect on FR nor modified the NA response.6. Vasopressin and histamine also failed to modify FR.7. Possibility of alpha-adrenoceptors in the neurones integrating FR is suggested.
TL;DR: Of several basic ethers of 3-alkyl-2,3-diphenylpropiophenones synthesized and evaluated in rats, three have been found to possess marked antiimplantation activity when given orally at a dose of 0.5 mg/kg body weight on days 1–5 post-coitum.
TL;DR: Biochemical changes in the ampulla, ampullary-isthmic junction, and the isthmus portions of the rabbit Fallopian tube have been investigated and it is suggested that the enzyme plays a role in denudation of ova and removal of cumulus and corona cell debris.
TL;DR: Synthetische Copolymere aus Glutaminsaure and Phenylalanin zeigen Lysozymaktivitat as mentioned in this paper, and mit einem Produkt Phe90Glu10 wurde ca.
Abstract: Synthetische Copolymere aus Glutaminsaure und Phenylalanin zeigen Lysozymaktivitat. Mit einem Produkt Phe90Glu10 wurde ca. ein Drittel der Lysozymaktivitat erreicht.
TL;DR: Micro doses of megestrol acetate were administered to 16 rats for 1 year to determine the effect on the genital organs and female fertility and the factors contributing to pregnancy failure were inhibition of mating, implantation failure and fetal resorption.
TL;DR: In this paper, the Michael reaction of diethyl (substituted amino)-methylenemalonate with hydrazine hydrate gave either 4-substitized 1,2,4-triazoles or 4-carbethoxy-5-hydroxy 4H-pyrazole, depending on the nature of the leaving group in the initially formed adduct.
TL;DR: It is suggested that a depression of metabolic status of the uterus by the progestogen is crucially involved in implantation failure and fetal resorption.
TL;DR: Sensitization with calciferol 24 hours before the injection of these salts causes consistent and selective calcification of the tubules, apparently unrelated to the calciphylactic property ofThese salts.
Abstract: A single intratesticular injection of potassium permanganate (0.08 mMol/kg body weight) causes selective calcification of the seminiferous tubules of the rat; aluminium chloride, chromium chloride, ferric chloride and ferrous sulphate are ineffective at the same dose even though all 5 evoke marked degenerative changes in the tubules and the interstitium. However, sensitization with calciferol (1 mg/100 g body weight, a single oral administration) 24 hours before the injection of these salts causes consistent and selective calcification of the tubules. Degenerative changes in the tubules and the interstitium are apparently unrelated to the calciphylactic property of these salts.
TL;DR: Treatment of the Thailand strain with quinine and the Panama-D strain with chloroquine, to which the strains are sensitive, eliminated rings and reduced the RNA and DNA in persisting gametocytes.
TL;DR: In this article, an intrauterine contraceptive device did not evoke any noteworthy histologic or histochemical changes in the rhesus monkey uterus and the Fallopian tube after continuous residence for 4 ½ years.
TL;DR: Hill soils are revealed to be superior to alluvial and lateritic soils in the harboured to ta l number of active cultures, and most of the active cultures exhibited a narrow spect rum of antibiotic act ivi ty and were found to inhibit either Gram positive bacter ia or fungi or both.
Abstract: Very little is known about the distribut ion of antagonistic act inomycetes in Indian soils. In view of this, work was under taken to elucidate the nature and population of antagonistic act inomycetes isolated from three types of Indian soils viz., hill, alluvial and lateritic soils (Roychowdhury et al., 1963). The soil samples were collected from gardens, road sides, manure dumps, forests and cult ivated fields. Thir ty hill soil samples (pH 5.5 to 5.8) were collected from the Kumaon region (Himalayan foot hills), 13 alluvial soil samples (pH 7.0 to 9.0) were collected from the Lucknow district (Indo-gangetic plain), and 11 lateriticsoils (pH 5.5 to 6.5)were collected from Mahabaleswar (Western Ghats). The climate of Lucknow is arid and tha t of the remaining two regions is humid. The act inomycetes were isolated b y the soil dilution plate method using Conn's agar medium (sodium asparaginate 0.1%; glycerol -1.0%; K2HPO 4 -1.0%; agar -3.0% and distilled water, p H 7.2 to 7.4) and organic agar medium (peptone -0.5~ meat ext ract -0.15 o/0; dextrose -0.1 ~/o; rodium chloride -0.35% and distilled water p H 7.2 to 7.4) and incubated for a period of 7-10 days at 28 C. Individual act inomycete colonies were picked up on the basis of colour of aerial mycelium, substrate mycelium and soluble p igment and maintained on Conn's and asparagine dextrose agar slants. The pr imary screening for antibiotic production of all the isolated colonies was made by adopting the spectrum plate method of Pridham et al., (1956), using .Bacillus subtills, Staphylococcus aureus, Corynebacterium tritici, Escherichia coli, Salmonella typhi, Candida albicans, Cryptococcus neoformans and Saccharomyces cerevisiae as test organisms. The results of pr imary screening have been tabula ted in Table 1. A close examination of the tabu la ted results reveals hill soils to be superior to alluvial and lateritic soils in the harboured to ta l number of active cultures. Most of the active cultures exhibited a narrow spect rum of antibiotic act ivi ty and were found to inhibit either Gram positive bacter ia or fungi or both. Very few were found to inhibit Gram positive and Gram negative bacteria, and none inhibited Gram negative bacteria exclusively. The number of fungal antagonists was found to be lower in alluvial soil than in hill and lateritic soils. I t has been noted tha t the p H of alluvial soils is neutral or alkaline whereas tha t of hill and lateritie soils is acid. The frequent occurrence of fungi in acid soils has been commented on by Kuster and Williams (1964). K r z y m y